BACLOFEN

Baclofen (BAC) is used to treat spasticity but has a short half-life of 2 to 4 hours, requiring multiple administrations per day. The study aimed to develop modified-release tablets to overcome this problem. 3 batches of tablets containing BAC were produced: F1 containing hydroxyethyl cellulose (HEC), F2 containing poloxamer (PF127) and F3 containing the polymeric mixture of HEC and PF127. The compatibility study was carried out using thermal analysis and infrared spectroscopy with Fourier transform. Powder quality control was obtained by averaging the weight, hardness, friability, disintegration, and in vitro release of the tablets. Compatibility studies by differential thermal analysis showed that the disappearance of the second BAC event by starch was observed, and the incompatibility was confirmed by the decrease in the intensity of the 3250 cm-1 band, which suggests O-H bonding. Colloidal silicon presented dioxide in the 1:1 binary mixture, suppression of all events, which may correspond to the suppression of band 2863 cm-1, referring to N-H stretching, and 2683 cm-1, which suggests an O-H bond of the carboxylic acid. The powder flow was unsatisfactory, so granulation was produced by the wet method. The hardness of the batches varied from 9.90 N to 29.70 N. Furthermore, the uniformity of content followed the Acceptance Values. The in vitro release study demonstrated that F2 was able to modify BAC release. However, it is necessary to change the development conditions.

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Publication Details

Journal
BIOFARM - Journal of Biology & Pharmacy and Agricultural Management
Published
2025-04-04
DOI
https://doi.org/10.18391/biofarm.v20i1.4421
Primary Topic
Botulinum Toxin and Related Neurological Disorders
Type
article
Field-Weighted Citation Impact
0.00

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article

BACLOFEN

João Augusto Oshiro, Sara Efigênia Dantas de Mendonça y Araújo, Milena Nogueira da Silva, Ana Cláudia Dantas de Medeiros
BIOFARM - Journal of Biology & Pharmacy and Agricultural Management
Botulinum Toxin and Related Neurological Disorders
article

BACLOFEN

João Augusto Oshiro, Sara Efigênia Dantas de Mendonça y Araújo, Milena Nogueira da Silva, Ana Cláudia Dantas de Medeiros
article en

Abstract

Baclofen (BAC) is used to treat spasticity but has a short half-life of 2 to 4 hours, requiring multiple administrations per day. The study aimed to develop modified-release tablets to overcome this problem. 3 batches of tablets containing BAC were produced: F1 containing hydroxyethyl cellulose (HEC), F2 containing poloxamer (PF127) and F3 containing the polymeric mixture of HEC and PF127. The compatibility study was carried out using thermal analysis and infrared spectroscopy with Fourier transform. Powder quality control was obtained by averaging the weight, hardness, friability, disintegration, and in vitro release of the tablets. Compatibility studies by differential thermal analysis showed that the disappearance of the second BAC event by starch was observed, and the incompatibility was confirmed by the decrease in the intensity of the 3250 cm-1 band, which suggests O-H bonding. Colloidal silicon presented dioxide in the 1:1 binary mixture, suppression of all events, which may correspond to the suppression of band 2863 cm-1, referring to N-H stretching, and 2683 cm-1, which suggests an O-H bond of the carboxylic acid. The powder flow was unsatisfactory, so granulation was produced by the wet method. The hardness of the batches varied from 9.90 N to 29.70 N. Furthermore, the uniformity of content followed the Acceptance Values. The in vitro release study demonstrated that F2 was able to modify BAC release. However, it is necessary to change the development conditions.

BIOFARM - Journal of Biology & Pharmacy and Agricultural ManagementVol. 20(1)
Universidade Estadual da Paraíba (BR)
Coordenação de Aperfeiçoamento de Pessoal de Nível Superior
Openalex Percentile: Top 65%
Botulinum Toxin and Related Neurological Disorders
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